HPLC法测定绞股蓝总苷胶囊中绞股蓝皂苷B的含量

目的:建立反相高效液相色谱法测定绞股蓝总苷胶囊中绞股蓝皂苷B的含量。方法:采用Agilent Eclipse XDB-C18色谱柱(250 mm×4.6 mm,5μm),以乙腈-0.5%磷酸(38∶62)为流动相,流速1.0 mL.min-1,检测波长210 nm,柱温30℃。结果:绞股蓝皂苷B进样量在0.04～2.0μg范围内,与峰面积呈良好线性关系;平均回收率(n=6)为102.1%,RSD为1.2%。结论:该方法简便、准确,重复性好,可作为绞股蓝总苷胶囊的质量控制方法。     

复方降糖滴丸质量标准研究

目的建立复方降糖滴丸的质量标准。方法采用薄层色谱法对滴丸中的栀子、绞股蓝进行定性鉴别,HPLC测定滴丸中栀子苷的含量,采用UV分别测定绞股蓝总皂苷和总多糖的含量。结果定性鉴别结果斑点圆整,分离度好,易于鉴别;栀子苷的线性范围为3.99~255.20μg.mL-1,r=0.999 8,回收率为99.4%,RSD为2.9%;绞股蓝总皂苷的线性范围为17.00~134.00μg.mL-1,r=0.999 5,回收率为98.4%,RSD为2.9%;绞股蓝总多糖线性范围为12.56~62.80μg.mL-1,r=0.999 3,回收率为98.9%,RSD为2.4%。结论本试验首次建立了复方降糖滴丸的质量标准,方法简便、准确、专属性强,可用于复方降糖滴丸的质量控制。     

绞股蓝总苷片的指纹图谱及含量测定

目的采用超高效液相色谱法建立中药制剂绞股蓝总苷片的指纹图谱,并同时测定其中人参皂苷Rb1和绞股蓝皂苷XLIX的含量。方法采用Kromat Universil XB C18色谱柱(150 mm×2.1mm,3μm),以乙腈-水为流动相进行梯度洗脱,流速为0.2mL·min-1,检测波长为203nm,柱温为30℃;建立绞股蓝总苷片指纹图谱,运用中国药典委员会"中药色谱指纹图谱相似度评价系统软件"对10批制剂进行相似度评价,并对其中2个色谱峰进行指认及含量测定。结果 10批绞股蓝总苷片指纹图谱中标定了17个共有色谱峰,相似度值为0.983~0.995。人参皂苷Rb1和绞股蓝皂苷XLIX质量浓度分别在4.2~42.0mg·L-1和9.4~94.0mg·L-1内与峰面积呈良好的线性关系,平均回收率分别为98.5%和99.4%。结论用该方法所建立的皂苷类指纹图谱方法,结合有关成分的含量测定能更好地控制其质量,对提高绞股蓝总苷片的整体质量控制提供参考依据。     

复方绞股蓝胶囊质量标准研究

目的建立复方绞股蓝胶囊的质量控制方法。方法采用薄层色谱法对绞股蓝进行定性鉴别,采用高效液相色谱法测定野黄芩苷的含量。结果绞股蓝的薄层色谱图斑点清晰,阴性对照品溶液无干扰;野黄芩苷对照品溶液质量浓度在0.007～0.1800 g/L范围内与峰面积线性关系良好,r=0.99994(n=6),平均回收率为99.01%,RSD=1.81%(n=6)。结论所用方法分离度好,快速、简便,可作为复方绞股蓝的质量控制方法。     

绞股蓝胶囊中绞股蓝总皂苷的稳定性研究

目的 对绞股蓝胶囊中绞股蓝皂苷的稳定性进行研究从而对本品质量进行控制.方法 采用恒温加速试验法.结果 准确地测定了绞股蓝胶囊中绞股蓝皂苷的稳定性.结论 本实验方法简便易行、速度快、稳定性好、RSD为2.48%;其回收率为100.71%、RSD为2.32%;经统计学处理和作图计算在室温(25℃)绞股蓝胶囊中绞股蓝总皂苷的有效期(1.63年)     

银杏绞股蓝胶囊的质量控制

目的:制定银杏绞股蓝胶囊的质量控制方法。方法:采用HPLC法测定银杏绞股蓝胶囊中含有的银杏总黄酮醇苷和人参皂苷Rb₁的含量;通过急性毒性实验验证银杏绞股蓝胶囊的安全用量。结果:HPLC法测得总黄酮醇苷中槲皮素、山柰素、异鼠李素进样量分别在0.06～0.75μg（r=0.9999）、0.06～0.75μg（r=0.9998）、0.04～0.50μg（r=0.9998）范围内与峰面积呈良好的线性关系,平均加样回收率分别为99.12%,98.96%,98.66%;HPLC梯度洗脱法测定绞股蓝总苷中人参皂苷Rb₁的含量,Rb1在进样量0.4～8.0μg（r=0.9996）范围内与峰面积呈良好的线性关系,平均加样回收率分别为96.98%;银杏绞股蓝胶囊口服途径的小鼠LD₅₀大于3 200mg·kg^-1,表明在临床常用剂量下是安全的。结论:建立的HPLC方法简便可行,准确可靠,可用于该胶囊的质量控制。     

绞股蓝总苷的药理作用及其临床应用进展

绞股蓝为葫芦科绞股蓝属植物,其主要药效成分为绞股蓝总皂苷。本文通过对大量绞股蓝总苷相关文献进行总结归纳,得出绞股蓝总苷具有降血脂、降血糖、心血管活性、改善记忆、抗组织纤维化、抗肿瘤等药理作用,临床可用于治疗高血脂症、老年脑血管性痴呆、肿瘤等疾病。绞股蓝总苷为葫芦科植物绞股蓝Gynostemma pentephyllum （ Thunb．） Mak．全草中提取得到的总皂苷经精制而成。     

基于HPLC-QAMS法同时测定清肺散结丸中阿克苷、苦玄参苷ⅠB、苦玄参苷ⅠA、三七皂苷R1、绞股蓝皂苷XLⅨ、绞股蓝皂苷A和绞股蓝皂苷ⅩⅦ的含量

摘要：目的:建立高效液相一测多评法同时测定清肺散结丸中阿克苷、苦玄参苷ⅠB、苦玄参苷ⅠA、三七皂苷R1、绞股蓝皂苷ⅩLⅨ、绞股蓝皂苷A和绞股蓝皂苷ⅩⅦ的含量。方法:采用高效液相一测多评法,以Welch Material C18（250 mm×4.6 mm,5μm）为色谱柱,柱温:25℃;流动相为乙腈-0.2%冰醋酸水溶液,梯度洗脱,流速为0.9 ml·min-1;检测波长分别为264 nm（检测阿克苷、苦玄参苷ⅠB和苦玄参苷ⅠA）和203 nm（检测三七皂苷R1、绞股蓝皂苷XLⅨ、绞股蓝皂苷A和绞股蓝皂苷ⅩⅦ）。以苦玄参苷ⅠA为内参物,建立其与阿克苷、苦玄参苷ⅠB、三七皂苷R1、绞股蓝皂苷XLⅨ、绞股蓝皂苷A和绞股蓝皂苷ⅩⅦ的相对校正因子,计算各成分含量。结果:阿克苷、苦玄参苷ⅠB、苦玄参苷ⅠA、三七皂苷R1、绞股蓝皂苷XLⅨ、绞股蓝皂苷A和绞股蓝皂苷ⅩⅦ分别在1.87～46.75μg·ml-1（r=0.999 1）、2.03～50.75μg·ml-1（r=0.999 7）、1.06～26.50μg·ml-1（r=0.999 3）、0.97～24.25μg·ml-1（r=0.999 6）、0.81～20.25μg·ml-1（r=0.999 1）、1.39～34.75μg·ml-1（r=0.999 7）、2.26～56.50μg·ml-1（r=0.999 5）范围内线性关系良好;平均加样回收率（RSD）分别为98.83%（0.97%）,100.11%（0.62%）,97.92%（1.38%）,96.96%（1.40%）,97.74%（1.18%）,99.15%（0.89%）和99.36%（1.01%）（n=9）;一测多评法的计算值与外标法（ESM）测定值间无明显差异。结论:所建立的HPLC-QAMS法结果准确,可用于清肺散结丸的质量控制。     

正交实验优选绞股蓝总皂苷的提取方法

采用分光光度法测定湘西野生七叶绞股蓝及其茶制品中绞股蓝总苷含量。设计正交实验考察不同提取方法对测定结果的影响 ,结果表明 8倍量的80 %甲醇回流 3次 ,每次 2 h为最佳提取方案     

绞股蓝总苷与辛伐他汀治疗原发性高脂血症的疗效比较

目的 以辛伐他汀为对照，观察绞股蓝总苷对高脂血症的疗效和安全性。方法 将60例患者随机分成绞股蓝总苷组（A组）30例和辛伐他汀组（B组）30例，治疗12周后比较调脂疗效、不良反应。结果 绞股蓝总苷及辛伐他汀均能明显降低血清总胆固醇（TC）、甘油三脂（TG）、低密度脂蛋白胆固醇（LDL-c）水平（P〈0．01），均能升高高密度脂蛋白胆固醇（HDL-c）水平（P〈0．05），不良反应较小。结论 绞股蓝总苷调脂疗效确切且不良反应少，值得临床推广。     

Efficacy of gut lavage,hemodialysis, and hemoperfusion in the therapy of paraquat or diquat intoxication

Clinical and in vitro investigations were carried out to test the efficacy of gut lavage, hemodialysis, and hemoperfusion in the treatment of poisoning with paraquat or diquat. In a patient suffering from diquat intoxication 130 times more diquat was removed by gut lavage 30 h after ingestion than was removed by complete aspiration of the gastric contents.Determination of in vitro clearances for paraquat and diquat by hemodialysis showed that, at serum concentrations of 1–2 ppm, such as are frequently encountered in poisoning in man, toxicologically relevant quantities of herbicide cannot be removed from the body. At a concentration of 20 ppm, on the other hand, hemodialysis proved to be effective, the clearance being 70 ml/min at a blood flow rate of 100 ml/min. The efficacy of hemoperfusion with coated activated charcoal was on the whole better. Especially at concentrations around 1–2 ppm, the clearance values for hemoperfusion were some 5–7 times higher than those for hemodialysis.In a patient suffering from paraquat poisoning, both hemodialysis as well as hemoperfusion were carried out. The in vitro results could be confirmed: At serum concentrations of paraquat less than 1 ppm no clearance could be obtained by hemodialysis while by hemoperfusion with activated charcoal quite high clearance values were measured and the serum level dropped down to zero.

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Zusammenfassung Klinische Untersuchungen und Laboratoriumsversuche wurden durchgeführt, um die Wirksamkeit von Darmspülung, Hämodialyse und Hämoperfusion bei Paraquat- und Deiquat-Vergiftungen zu prüfen.Bei einem Patienten wurde 30 Std nach Deiquat-Aufnahme durch Darmspülung 130mal mehr Deiquat entfernt als durch vollständige Aspiration des Mageninhaltes. In vitro-Versuche ergaben, daß bei Blutserumkonzentrationen von 1–2 ppm, die bei Vergiftungen oft gemessen werden, durch Hämodialyse keine toxikologisch relevanten Paraquat- oder Deiquat-Mengen entfernt werden können. Dagegen erwies sich die Hämodialyse bei 20 ppm und einer Blutumlaufgeschwindigkeit von 100 ml/min mit einer Clearance von 70 ml/min als wirksam. Die Hämoperfusion mit beschicheter Aktivkohle war in diesen Versuchen aber eindeutig überlegen, denn insbesondere bei Konzentrationen um 1–2 ppm waren die Clearance-Werte 5–7mal höher als bei der Hämodialyse.Die in vitro-Ergebnisse wurden bei einem Patienten mit einer Paraquat-Vergiftung bestätigt: Bei Konzentrationen unter 1 ppm war die Hämodialyse wirkungslos, während durch Hämoperfusion relativ hohe Clearance-Werte erreicht wurden, so daß der Serumspiegel rasch unter die Nachweisgrenze abfiel.

     

In vitro studies on sterically stabilized liposomes (SL) as enzyme carriers in organophosphorus (OP) antagonism

This study describes a new approach for organophosphorous (OP) antidotal treatment by encapsulating an OP hydrolyzing enzyme, OPA anhydrolase (OPAA), within sterically stabilized liposomes. The recombinant OPAA enzyme was derived from Alteromonas strain JD6. It has broad substrate specificity to a wide range of OP compounds: DFP and the nerve agents, soman and sarin. Liposomes encapsulating OPAA (SL)* were made by mechanical dispersion method. Hydrolysis of DFP by (SL)* was measured by following an increase of fluoride ion concentration using a fluoride ion selective electrode. OPAA entrapped in the carrier liposomes rapidly hydrolyze DFP, with the rate of DFP hydrolysis directly proportional to the amount of (SL)* added to the solution. Liposomal carriers containing no enzyme did not hydrolyze DFP. The reaction was linear and the rate of hydrolysis was first order in the substrate. This enzyme carrier system serves as a biodegradable protective environment for the recombinant OP-metabolizing enzyme, OPAA, resulting in prolongation of enzymatic concentration in the body. These studies suggest that the protection of OP intoxication can be strikingly enhanced by adding OPAA encapsulated within (SL)* to pralidoxime and atropine.     

Aquatic Insects and Trace Metals: Bioavailability,Bioaccumulation, and Toxicity

Abstract

The uptake of metals from food and water sources by insects is thought to be additive. For a given metal, the proportions taken up from water and food will depend both on the bioavailable concentration of the metal associated with each source and the mechanism and rate by which the metal enters the insect. Attempts to correlate insect trace metal concentrations with the trophic level of insects should be made with a knowledge of the feeding relationships of the individual taxa concerned. Pathways for the uptake of essential metals, such as copper and zinc, exist at the cellular level, and other nonessential metals, such as cadmium, also appear to enter via these routes. Within cells, trace metals can be bound to proteins or stored in granules. The internal distribution of metals among body tissues is very heterogeneous, and distribution patterns tend to be both metal and taxon specific. Trace metals associated with insects can be both bound on the surface of their chitinous exoskeleton and incorporated into body tissues. The quantities of trace meals accumulated by an individual reflect the net balance between the rate of metal influx from both dissolved and particulate sources and the rate of metal efflux from the organism. The toxicity of metals has been demonstrated at all levels of biological organization: cell, tissue, individual, population, and community. Much of the literature pertaining to the toxic effects of metals on aquatic insects is based on laboratory observations and, as such, it is difficult to extrapolate the data to insects in nature. The few experimental studies in nature suggest that trace metal contaminants can affect both the distribution and the abundance of aquatic insects. Insects have a largely unexploited potential as biomonitors of metal contamination in nature. A better understanding of the physico-chemical and biological mechanisms mediating trace metal bioavailability and exchange will facilitate the development of general predictive models relating trace metal concentrations in insects to those in their environment. Such models will facilitate the use of insects as contaminant biomonitors.     

Alzheimer’s disease – current trends in basic and clinical research. Highlights from the 16th ECNP

Advances in the molecular biological knowledge of neuronal nicotinic acetylcholine receptors (nAChRs) have led to a growing interest by the pharmaceutical industry in the development of novel compounds that selectively modulate nAChR function. The ability of (-)-nicotine, an activator of nAChRs, to enhance attentional aspects of cognition in animals and humans, to exert neuroprotective and anxiolytic-like effects, and presumably to mediate the negative correlation between smoking and Alzheimer's (and Parkinson's) Disease, has focused interest on the potential therapeutic utility of modulators of nAChR function for treatment of some of the deficits associated with these progressive, neurodegenerative conditions. Numerous compounds are known which activate nAChRs and which might serve as lead compounds toward the development of such agents. The pharmacologic diversity of neuronal nAChR subtypes suggests the possibility of developing selective compounds which would have more favourable side-effect profiles than existing agents. This broader class of agents, collectively called cholinergic channel modulators (ChCMs), is anticipated to encompass compounds which would have more favourable side-effect profiles than existing agents, which generally exhibit low selectivity. This selectivity may be achieved by preferentially activating some subtypes of nAChRs (i.e., Cholinergic Channel Activators, ChCAs) or inhibiting the function of other subtypes (Cholinergic Channel Inhibitors, ChCIs). An overview of the biology of nAChRs and the rationale for the use of ChCMs for the treatment of dementia related to neurodegenerative diseases are presented, followed by a discussion of lead compounds and compounds under consideration for clinical evaluation.     

Steroidal sapogenin contents in some domestic plants

In order to find out the values of the steroid resources for the future use. the compositions and contents of steroidal sapogenins from 13 domestic plants have been investigated. As a result,Dioscorea nipponica, D. quinqueloba andSmilax china were found to have large amount of diosgenin. And pennogenin inTrillium kamtschaticum andParis verticillata, yuccagenin inAllium fistulosum, hecogenin inAgave americana and neochlorogenin inSolanum nigum were appeared to be major steroidal sapogenins.